Design, synthesis and activities of aziridine derivatives of N5-methyltetrahydrofolate against methionine synthase
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  • 作者:Xiling Deng ; Ying Guo ; Chao Tian ; Junyi Liu…
  • 关键词:Aziridine ; Methionine synthase ; Ring closure reaction ; N5 ; Methyltetrahydrofolate
  • 刊名:Chemical Research in Chinese Universities
  • 出版年:2015
  • 出版时间:October 2015
  • 年:2015
  • 卷:31
  • 期:5
  • 页码:742-745
  • 全文大小:459 KB
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  • 作者单位:Xiling Deng (1) (3)
    Ying Guo (1)
    Chao Tian (1)
    Junyi Liu (1) (2)
    Xiaowei Wang (1)
    Zhili Zhang (1)

    1. School of Pharmaceutical Sciences, Peking University, Beijing, 100191, P. R. China
    3. School of Pharmaceutical Sciences, Shihezi University, Shihezi, 832000, P. R. China
    2. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, 100191, P. R. China
  • 刊物主题:Chemistry/Food Science, general; Analytical Chemistry; Inorganic Chemistry; Organic Chemistry; Physical Chemistry;
  • 出版者:Springer Berlin Heidelberg
  • ISSN:2210-3171
文摘
Aziridine derivatives of N5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 and 6 exhibited superior inhibitory activities(IC50: 5.05 and 4.15 μmol/L, respectively) compared to the corresponding chain analogue 4(IC50=24.42 μmol/L). The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase. Keywords Aziridine Methionine synthase Ring closure reaction N5-Methyltetrahydrofolate

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